6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.

Abstract Investigation of a series 6-[2-(4-aryl-1-piperazinyl)ethyl]-2 H -1,4-benzoxazin-3(4 H )-ones has led to the discovery of potent 5-HT 1A/1B/1D receptor antagonists with and without additional SerT affinity. Modulation of the different target activities gave compounds with a range of profiles suitable for further in vivo characterization.